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槲皮素舒张大鼠离体肾动脉及其与L-型电压依赖性钙通道和蛋白激酶C的关系

侯晓敏¹, 张明升², 秦小江^2,*

¹山西医科大学基础医学院，太原 030001；²山西医科大学公共卫生学院，太原 030001

摘要

为了观察槲皮素对大鼠离体肾动脉的舒张作用，并探讨该作用与蛋白激酶C (protein kinase C, PKC)的关系，本研究采用血管张力测定仪记录大鼠肾动脉肌张力变化，用膜片钳全细胞记录方式记录大鼠肾动脉血管平滑肌细胞(vascular smooth muscle cell, VSMC) L-型电压依赖性钙通道(L-type voltage-gated Ca²⁺ channels, LVGC)电流。实验结果显示，槲皮素能够舒张60 mmol/L KCl或 1 × 10−5 mol/L 苯肾上腺素(phenylephrine, PE)预收缩的大鼠肾动脉，其最大舒张百分比分别为(84.53 ± 7.35)%和(76.42 ± 4.63)%；血管内皮完整组和去内皮组肾动脉相比，槲皮素对预收缩肾动脉的最大舒张百分比没有显著性差异；预孵育PKC特异性抑制剂C6303可使槲皮素对肾动脉的最大舒张幅度降低，与未孵育C6303组相比具有统计学差异(P < 0.05)；离体大鼠肾动脉VSMC的正常LVGC尖峰电流密度为(23.17 ± 1.33) pA/pF，10 μmol/L槲皮素可以降低其电流密度到(10.46 ± 1.35) pA/pF，其抑制百分比为54.86%，1 μmol/L C6303可部分逆转槲皮素对LVGC电流的降低幅度，其抑制百分比为62.08% (P < 0.05)。上述实验结果提示，槲皮素可舒张大鼠离体肾动脉，该作用具有浓度依赖性且不受内皮影响，可能与抑制LVGC和激活PKC有关。

关键词： 槲皮素; 肾动脉 ; 舒张 ; L-型电压依赖性钙通道 ; 蛋白激酶C

分类号：R322

Vasodilation of quercetin on rat renal artery and the relationship with L-type voltage-gated Ca²⁺ channels and protein kinase C

HOU Xiao-Min¹, ZHANG Ming-Sheng², QIN Xiao-Jiang^2,*

¹School of Basic Medical Sciences, Shanxi Medical University, Taiyuan 030001, China；²School of Public Health, Shanxi Medical University, Taiyuan 030001, China

Abstract

To investigate the diastolic function of quercetin on rat renal artery in vitro and its mechanism, the tension of rat renal artery was recorded by multi myograph system, and the L-type voltage-gated Ca²⁺ channels (LVGC) current was recorded by whole-cell patch clamp technique. Quercetin produced relaxation effect on rat renal artery pre-contracted by 60 mmol/L KCl or 1 × 10−5 mol/L phenylephrine, and the maximal diastolic percentage was  (84.53 ± 7.35)% or (76.42 ± 4.63)%. There was no statistical difference in the maximal diastolic percentage between endothelium-intact and endothelium-denuded groups. Pre-incubation of protein kinase C (PKC) inhibitor C6303 inhibited the maximal diastolic amplitude induced by quercetin. The peak current density of LVGC in rat renal artery vascular smooth muscle cells (VSMCs) was (23.17 ± 1.33) pA/pF. Quercetin (10 μmol/L) inhibited the peak current to (10.46 ± 1.35) pA/pF, and the inhibition percentage was 54.86%. C6303 (1 μmol/L) partially reversed the inhibitory effect of quercetin, and the inhibition percentage was 62.08% (P < 0.05). These results suggest that quercetin can relax rat renal artery in vitro in a concentration-dependent and endothelium- independent manner. The vasodilation of quercetin may be related to inhibition of LVGC current and activation of PKC.

Key words: quercetin; renal artery ; relaxation ; L-type voltage-gated Ca2+ channels ; protein kinase C

收稿日期：2017-05-03　　录用日期：2017-10-13

通讯作者：秦小江　　E-mail: sxykdxyxy@163.com

DOI: 10.13294/j.aps.2017.0079

引用本文：

侯晓敏, 张明升, 秦小江. 槲皮素舒张大鼠离体肾动脉及其与L-型电压依赖性钙通道和蛋白激酶C的关系[J]. 生理学报 2017; 69 (6): 775-780.

HOU Xiao-Min, ZHANG Ming-Sheng, QIN Xiao-Jiang. Vasodilation of quercetin on rat renal artery and the relationship with L-type voltage-gated Ca²⁺ channels and protein kinase C. Acta Physiol Sin 2017; 69 (6): 775-780 (in Chinese with English abstract).